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Assay Detail

CHEMBL822530

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of saturable binding of [3H]idazoxan to alpha2-site in rat cerebral cortical membranes.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Indoline analogues of idazoxan: potent alpha 2-antagonists and alpha 1-agonists.
Fagan GP, Chapleo CB, Lane AC, Myers M, Roach AG, Smith CF, Stillings MR, Welbourn AP.
J Med Chem (1988) 31 : 944 -948
PubMed 2896247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.18 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL556758 1 9.80
CHEMBL36616 1 9.62
CHEMBL172132 1 9.38
CHEMBL38829 1 9.16
CHEMBL38788 1 9.02
CHEMBL289153 1 8.73
CHEMBL537841 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL556758 Ki = 0.16 nM 9.80
CHEMBL36616 Ki = 0.24 nM 9.62
CHEMBL172132 Ki = 0.42 nM 9.38
CHEMBL38829 Ki = 0.69 nM 9.16
CHEMBL38788 Ki = 0.96 nM 9.02
CHEMBL289153 Ki = 1.87 nM 8.73
CHEMBL537841 Ki = 3.0 nM 8.52